TABLE 2

PK and CNS penetration of capecitabine and 5-FU after oral administration of capecitabine at 400 mg/kg to BALB/c mouse

Compound	PK Parameter	Matrix			CNS Penetration
Compound	PK Parameter	Blood	Brain	CSF	K_p,brain^a	K_p,CSF^a	K_p,uu,brain^b	K_p,uu,CSF^b
Capecitabine	T_max (hour)	0.25	0.16	0.25	—	—	—	—
	C_max (ng/ml)	64,000	2406	7677	—	—	—	—
	AUC_0−t (ng·h/ml)	33,615	1482	4494	0.04	0.13	0.03	0.23
	AUC_0−inf (ng·h/ml)	33,643	1484	4726	0.04	0.14	0.03	0.25
5-FU	T_max (hour)	0.50	0.50	0.50	—	—	—	—
	C_max (ng/ml)	315	25.9	40.3	—	—	—	—
	AUC_0−t (ng·h/ml)	335	50.7	42.7	0.15	0.13	0.12	0.27
	AUC_0−inf (ng·h/ml)	338	57.5	46.1	0.17	0.14	0.13	0.29

↵^a K_p,brain = AUC_brain/AUC_blood; K_p,CSF = AUC_CSF/AUC_blood.
↵^b K_p,uu,brain = K_p,brain × f_u,brain/f_u,blood; K_p,uu,CSF = K_p,CSF/f_u,blood.
—not relevant for the calculation of CNS penetration